艾司洛尔盐酸盐的新合成方法  

A new synthesis method of esmolol hydrochloride

作　　者：贺正国 蒋琳 江登榜 岳越 李树生 袁明伟 HE Zheng-guo;JIANG Lin;JIANG Deng-bang;YUE Yue;LI Shu-sheng;YUAN Ming-wei(School of Chemistry and Environment,National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials,Yunnan Minzu University,Kunming 650504,Yunnan,China;Yunnan Nanyi Biotechnology Co.LTD,Kunming 650300,Yunnan,China)

机构地区：[1]云南民族大学化学与环境学院,生物基材料绿色制备技术国家地方联合工程研究中心,云南昆明650504 [2]云南南益生物科技有限公司,云南昆明650300

出　　处：《云南大学学报（自然科学版）》2021年第5期985-989,共5页Journal of Yunnan University(Natural Sciences Edition)

基　　金：云南省“高层次人才引进计划”产业人才专项支持;国家自然科学基金(21302163);云南省基础研究专项—青年项目(202001AU070007).

摘　　要：艾司洛尔盐酸盐是一种超短效β1受体阻滞剂,在临床上主要用于室上性心动过速、围术期高血压,也可用于室上性快速性心律失常,特点是起效快,作用时间短.以4-溴苯酚为起始原料,经Heck反应、氢化、溴丙烯醚化、氧化、异丙胺开环、成盐6步反应合成艾司洛尔盐酸盐,总产率为46%,为艾司洛尔盐酸盐的合成提供了一条新的路线.Esmolol hydrochloride is an ultra-short actingβ1-receptor blocker,which has mainly used for supraventricular tachycardia and perioperative hypertension.It has been also used for supraventricular tachyarrhythmia in clinical practice.The drug is characterized by quick effect and short action time.In this paper using 4-bromophenol as a starting material,esmolol hydrochloride was prepared by Heck reaction with methyl acrylate,hydrogenation,etherification with 3-bromopropene,oxidation,then isopropylamine was used to open the epoxide and salinization,the overall yield of the 6 synthetic steps is 46%.This method provides a new synthetic route for the synthesis of esmolol hydrochloride.

关 键 词：艾司洛尔盐酸盐 Β1受体阻滞剂 心律失常 HECK反应 氧化 

分 类 号：O625.52[理学—有机化学]